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Open Access Molecular Design of Synthetic Benzimidazoles for the Switchover of the Duplex to G-quadruplex DNA Recognition

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Benzimidazole derivatives are well known for their antibacterial, antiviral, anticonvulsant, antihistaminic, anthelmintic and antidepressant activities. Benzimidazole's unique base-selective DNA recognition property has been studied widely. However, most of the early benzimidazole systems have been targeted towards the binding of duplex DNA. Here we have shown the evolution and progress of the design and synthesis of new benzimidazole systems towards selective recognition of the double-stranded DNA first. Then in order to achieve selective recognition of the G-quadruplex DNA and utilize their potential as future anti-cancer drug candidates, we have demonstrated their selective cytotoxicity towards the cancer cells and potent telomerase inhibition ability.
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Keywords: ANTI-CANCER; BENZIMIDAZOLE; CYTOTOXICITY; DNA; G-QUADRUPLEX; TELOMERASE; TRAP-LIG ASSAY

Document Type: Research Article

Affiliations: 1: Department of Organic Chemistry Indian Institute of Science Bangalore 560012, India 2: Department of Organic Chemistry Indian Institute of Science Bangalore 560012, India; Chemical Biology Unit Jawaharlal Nehru Centre for Advanced Scientific Research Bangalore 560012, India; J.C. Bose Fellow, Department of Science and Technology New Delhi, India. [email protected]

Publication date: February 1, 2013

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  • International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions

    CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.

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